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10 sources retrieved · Most recent: April 2026 · Index updated 15 days ago
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HCAR1
hydroxycarboxylic acid receptor 1
Chromosome 12 · 12q24.31
NCBI Gene: 27198Ensembl: ENSG00000196917.6HGNC: HGNC:4532UniProt: A0A4Y1JWP1
49PubMed Papers
20Diseases
0Drugs
0Pathogenic Variants
FUNCTIONAL ROLE
Receptor
DATA QUALITY
✓ Experimental GO Evidence✓ Swiss-Prot Reviewed
G protein-coupled receptor activityprotein bindingadenylate cyclase-inhibiting G protein-coupled receptor signaling pathwaynegative regulation of lipid catabolic processbreast cancerneoplasmcancerSepsis
✦AI Summary

HCAR1 (also known as GPR81) is a G-protein-coupled receptor that serves as the primary cellular receptor for lactate, mediating diverse physiological and pathological processes through Gi-protein signaling pathways 12. The receptor plays a crucial role in metabolic regulation, where lactate binding activates anti-lipolytic effects and influences energy metabolism 1. In cancer biology, HCAR1 contributes to tumor progression through multiple mechanisms: it drives cachexia by activating a Gi-Gβγ-RhoA/ROCK1-p38 signaling cascade in adipose tissue 1, promotes immunosuppression by inducing CCL2/CCL7 chemokine expression that recruits immunosuppressive myeloid-derived suppressor cells 3, and regulates ferroptosis resistance through AMPK-SCD1 pathway modulation 4. HCAR1 also mediates beneficial effects in tissue homeostasis, promoting intestinal stem cell proliferation and epithelial development through Wnt/β-catenin signaling 2. However, chr12 activation can be detrimental, as demonstrated in osteoarthritis where HCAR1 signaling promotes chondrocyte damage via PI3K/Akt-mediated NOX4 upregulation and oxidative stress 5. The receptor's involvement in exercise-induced angiogenesis suggests additional roles in vascular health 6. These findings highlight HCAR1 as a promising therapeutic target for cancer cachexia, immunotherapy resistance, and metabolic disorders.

Sources cited
1
HCAR1 mediates lactate-induced cachexia through Gi-Gβγ-RhoA/ROCK1-p38 signaling pathway in adipose tissue
PMID: 38499763
2
HCAR1 activation induces CCL2/CCL7 chemokine expression leading to recruitment of immunosuppressive PMN-MDSCs in colorectal cancer
PMID: 39905201
3
HCAR1 is required for lactate-mediated intestinal stem cell proliferation and epithelial development through Wnt/β-catenin signaling
PMID: 30543778
4
HCAR1/MCT1-mediated lactate uptake regulates ferroptosis resistance through AMPK-SCD1 pathway in hepatocellular carcinoma
PMID: 33296645
5
HCAR1 mediates lactate-induced chondrocyte damage through PI3K/Akt signaling and NOX4 upregulation in osteoarthritis
PMID: 37688977
6
HCAR1 increase is associated with exercise-induced angiogenesis in cerebral vessels
PMID: 37600508
Disease Associationsⓘ20
breast cancerOpen Targets
0.11Weak
neoplasmOpen Targets
0.11Weak
cancerOpen Targets
0.10Suggestive
SepsisOpen Targets
0.08Suggestive
osteoarthritisOpen Targets
0.08Suggestive
gastric cancerOpen Targets
0.08Suggestive
lung cancerOpen Targets
0.08Suggestive
colitisOpen Targets
0.08Suggestive
idiopathic pulmonary fibrosisOpen Targets
0.07Suggestive
familial hypobetalipoproteinemia 2Open Targets
0.06Suggestive
Abnormality of the skeletal systemOpen Targets
0.06Suggestive
apolipoprotein c-III deficiencyOpen Targets
0.06Suggestive
cholesterol-ester transfer protein deficiencyOpen Targets
0.05Suggestive
glioblastoma multiformeOpen Targets
0.05Suggestive
hypertriglyceridemia 2Open Targets
0.05Suggestive
Metaphyseal chondrodysplasia, Schmid typeOpen Targets
0.04Suggestive
Schmid metaphyseal chondrodysplasiaOpen Targets
0.04Suggestive
osteosarcomaOpen Targets
0.04Suggestive
Oral ulcerOpen Targets
0.04Suggestive
multiple epiphyseal dysplasia, with severe proximal femoral dysplasiaOpen Targets
0.04Suggestive
Pathogenic Variants
No pathogenic variants reported on ClinVar for this gene.
View on ClinVar ↗
Related Genes
HCAR3Shared pathway100%DENRProtein interaction84%HCAR2Shared pathway50%OXER1Shared pathway50%GPR146Shared pathway33%TAAR1Shared pathway25%
Tissue Expression6 tissues
Brain
100%
Ovary
40%
Heart
26%
Lung
26%
Liver
19%
Bone Marrow
10%
Gene Interaction Network
Click a node to explore
HCAR1HCAR3DENRHCAR2OXER1GPR146TAAR1
PROTEIN STRUCTURE
Preparing viewer…
PDB9IZD · 3.16 Å · EM
View on RCSB ↗
Constraintⓘ
LOEUFⓘ
1.77LoF Tolerant
pLIⓘ
0.38Tolerant
Observed/Expected LoF0.00 [0.00–1.77]
RankingsWhere HCAR1 stands among ~20K protein-coding genes
  • #8,952of 20,598
    Most Researched49
  • #16,453of 17,882
    Most Constrained (LOEUF)1.77
Genes detectedHCAR1
Sources retrieved10 papers
Response time—
📄 Sources
10▼
1
Exercise therapy to prevent and treat Alzheimer's disease.
PMID: 37600508
Front Aging Neurosci · 2023
1.00
2
Monocarboxylate transporters in cancer.
PMID: 31395464
Mol Metab · 2020
0.90
3
Activation of GPR81 by lactate drives tumour-induced cachexia.
PMID: 38499763
Nat Metab · 2024
0.80
4
The lactate receptor HCAR1 drives the recruitment of immunosuppressive PMN-MDSCs in colorectal cancer.
PMID: 39905201
Nat Immunol · 2025
0.70
5
Microbiota-Derived Lactate Accelerates Intestinal Stem-Cell-Mediated Epithelial Development.
PMID: 30543778
Cell Host Microbe · 2018
0.60